左旋延胡索乙素贴片及其体外经皮渗透研究

Preparation of L-tetrahydropalmatine transdermal patch and its release evaluation in vitro

目的:考察左旋延胡索乙素贴片体外经皮渗透,筛选贴片最佳处方。方法:采用Valia-Chien双室渗透扩散池进行体外经皮渗透实验,以大鼠离体皮肤为渗透屏障,以HPLC测定左旋延胡索乙素的浓度。通过药物累积渗透量筛选药物浓度、透皮促进剂种类及浓度。结果:左旋延胡索乙素贴片最佳处方含药量为6 mg·10 cm^(-2),月桂氮革酮浓度为20%,薄荷油浓度为15%,24 h平均累积渗透量为173.073μg·cm^(-2),渗透速率为7.818μg·cm^(-2)·h^(-1)。结论:左旋延胡索乙素贴片有望成为新的给药制剂。

Objective： To investigate the percutaneous permeability of 1-tetrahydropalmatine （L-THP） transdermal patch in vitro and optimize the formulations. Methods： Transdermal permeability of L-THP was carried out by using the Valia-Chien double-compartment permeation cell with isolated rat skin. The concentration of drug was determined by HPLC. Results： The optimal formulation of L-THP patch contained L-THP （6 mg· 10 cm^-2）, azone （20%） and peppermint oil （15%）. The accumulative permeation amount of L-THP patch was 173. 073 μg ·cm ^-2 in 24 h, and the penetration rate was 7. 818 μg· cm^-2 ·h^-1 Conclusion： 1-Tetrahydropalmatine transdermal patch would be developed as a novel transdermal preparation.